peptidechats
Research information only. Not medical advice. 18+ only. Not FDA-approved for human therapeutic use.

Eptifibatide

Also known as: Integrilin, GP IIb/IIIa inhibitor peptide, barbourin-derived cyclic heptapeptide, integrin αIIbβ3 antagonist

Cyclic heptapeptide; glycoprotein IIb/IIIa (integrin αIIbβ3) inhibitor; antiplatelet agent

Research chemicalLast updated: October 10, 2026
Ask about Eptifibatide in chat →

What it is

Eptifibatide (Integrilin) is an IV medication given in cardiac care units to prevent blood clots during and after procedures to open blocked heart arteries. Derived from rattlesnake venom, it works by temporarily blocking the proteins on platelets that cause them to clump together. FDA-approved since 1998.

The scientific side

eptifibatide exerts its antiplatelet effect by selectively and competitively blocking the platelet membrane glycoprotein (GP) IIb/IIIa receptor, also known as integrin αIIbβ3. This receptor represents the final common pathway for platelet aggregation: when activated, GP IIb/IIIa binds soluble fibrinogen and von Willebrand factor, forming cross-links between adjacent platelets and producing the platelet thrombus that underlies acute coronary syndromes. Eptifibatide was designed by mimicking barbourin, a GP IIb/IIIa-selective disintegrin found in the venom of the southeastern pygmy rattlesnake (Sistrurus miliarius barbouri). It is a cyclic heptapeptide containing a Lys-Gly-Asp (KGD) sequence that confers high selectivity for GP IIb/IIIa over other RGD-binding integrins such as αvβ3, distinguishing it from the non-selective agent abciximab. Binding of eptifibatide to the GP IIb/IIIa receptor is competitive and reversible: antiplatelet activity has a rapid onset (>80% inhibition of ADP-induced platelet aggregation within minutes of bolus dosing) and rapid offset after discontinuation, with platelet function recovering to near-baseline within 4–6 hours due to the drug's short plasma half-life of approximately 2.5 hours and primarily renal clearance. Pharmacokinetic studies in both healthy volunteers and patients with ischemic heart disease confirmed rapid reversibility of antihemostatic effect. Unlike abciximab, eptifibatide and tirofiban are classified as small-molecule specific GP IIb/IIIa inhibitors with off-target effects primarily limited to suppression of inflammatory responses; they do not cross-react with integrin αvβ3 or leukocyte integrin Mac-1. In the PURSUIT trial (n=10,948), eptifibatide reduced the composite endpoint of death or myocardial infarction at 30 days from 15.7% (placebo) to 14.2% (p=0.042), establishing the clinical relevance of GP IIb/IIIa blockade as the mechanism of benefit in ACS.

Class: Cyclic heptapeptide; glycoprotein IIb/IIIa (integrin αIIbβ3) inhibitor; antiplatelet agent

Administration & storage

Administration
Intravenous bolus injection from the 2 mg/mL vialfollowed by continuous IV infusion from the 0.75 mg/mL vial via infusion pumpAdministration through the same IV line as heparinIntracoronary administration has been studied but is not standard practice
Storage
Store vials refrigerated at 2–8°C (36–46°F). Protect from light. Discard any unused portion; single-use vials only. Once removed from refrigerator, may be stored at controlled room temperature for up to 2 months.
Cautions
Hospital-only, intravenous medication — not for use outside of monitored cardiac or critical care settings.,CONTRAINDICATED in severe renal impairment requiring dialysis (ESRD) — drug cannot be cleared adequately.,CONTRAINDICATED in patients with active internal bleeding or history of bleeding diathesis within prior 30 days.,CONTRAINDICATED in patients who have had a stroke within 30 days or any history of hemorrhagic stroke.,CONTRAINDICATED in concurrent use of another parenteral GP IIb/IIIa inhibitor.,CONTRAINDICATED in patients with thrombocytopenia (<100,000 platelets/µL).,Major bleeding risk: rates of 2.1% in ACS trials vs. 1.3% placebo; site of major bleeding most commonly arterial access site. Transradial approach reduces bleeding risk.,Eptifibatide-induced thrombocytopenia (EIT): rare (< 1% in clinical trials) but potentially severe immune-mediated drop in platelet count, sometimes occurring within hours but also reported as delayed-onset up to 5 days post-initiation. Requires immediate discontinuation and platelet monitoring. (PMIDs: 33813877, 37884759, 34127501, 33889336),Monitor platelet count, hemoglobin, hematocrit, serum creatinine, and PT/PTT prior to treatment and at 2–4 hours after initiation.,In patients receiving concomitant heparin, maintain aPTT 50–70 seconds and ACT 200–300 seconds during PCI to reduce bleeding risk while maintaining efficacy.

Legal & regulatory status

US FDA

FDA-approved (NDA) as Integrilin (eptifibatide) injection for (1) treatment of patients with acute coronary syndrome (ACS), including those to be managed medically and those undergoing percutaneous coronary intervention…

WADA

Eptifibatide is not listed on the WADA Prohibited List. It is a hospital-only intravenous antiplatelet agent with no known performance-enhancing application in sport and no documented misuse in athletic populations.

Health Canada

Eptifibatide (Integrilin) is approved in Canada for use in patients with acute coronary syndromes and in patients undergoing percutaneous coronary intervention, consistent with its FDA indications. Referenced in…